neutrophil elastase

Neutrophil elastase inhibitor 4 (compound 4f) is a competitive inhibitor of human neutrophil elastase (HNE) with IC50 of 42.30 nM and Ki of 8.04 nM. It prompts apoptosis in T47D cells and inhibits the proliferation of T47D, RPMI 8226, A549, and HSF cells with respective IC50 values of 21.25, 34.17, 29.93, and 99.11 nM [1].

BOS-318 is a Furin inhibitor with slowly dissociating, highly selective, and cell-pemeable characteristcs.

2-(2-bromophenyl)-5-chloro-4H-3,1-benzoxazin-4-one is an human neutrophil elastase inhibitor.

2-CHLOROMETHYL-1,1-DIOXO-1,2-DIHYDRO-1LAMBDA*6*-BENZO[D]ISOTHIAZOL-3-ONE targets the Neutrophil elastase (human).

AZD8309 is a potent, orally available antagonist of the chemokine receptor CXCR2 that regulates neutrophil transport, significantly reduces MPO in the pancreas and lung, and decreases trypsin and elastase activity in the pancreas.AZD8309 can be used to study a range of inflammatory diseases.

BAY-678 is a human neutrophil elastase (HNE; IC50: 20 nM) inhibitor with oral bioactivity, potency and selectivity.BAY-678 is a chemical probe recommended by the Structural Genomics Consortium (SGC).

GW-311616 hydrochloride is a long duration, orally bioavailable, and selective human neutrophil elastase (HNE) inhibitor (IC50: 22 nM; Ki: 0.31 nM).

SSR69071 is a potent, orally active, and selective inhibitor of neutrophil elastase. SSR69071 displays a higher affinity for human elastase (Ki =0.0168 nM) than for rat (Ki =3 nM), mouse (Ki =1.8 nM), and rabbit (Ki = 58 nM) elastases [2]. SSR69071 reduces myocardial infarct size following ischemia-reperfusion injury [1]. SSR69071 also has the potential for the treatment of chronic obstructive pulmonary diseases, asthma, emphysema, cystic fibrosis, and several inflammatory diseases.

MeOSuc-AAPA-CMK is a potent inhibitor of human neutrophil elastase (HNE) [1].

Cathepsin C-IN-6 (compound 2), an E-64c-hydrazideas-derived inhibitor of cathepsin C, possesses anti-inflammatory properties and impedes neutrophil elastase activation. This compound demonstrates potential efficacy in treating inflammatory diseases characterized by elevated neutrophil counts, such as chronic obstructive pulmonary disease (COPD) [1].

BAY-85-8501 is a selective, reversible and potent inhibitor of Human Neutrophil Elastase (HNE; IC50 of 65 pM)

Lodelaben is a human neutrophil elastase inhibitor with an IC50 and Ki of 0.5 and 1.5 μM, respectively.

FK706 is a slow-binding and competitive human neutrophil elastase inhibitor (IC50: 83 nM; Ki: 4.2 nM). FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase (IC50s: 22 nM and 100 nM, respectively). FK706 has an anti-inflammatory ef

AZD-9819 is an inhibitor of human neutrophil elastase for potential treatment of chronic obstructive pulmonary disease (COPD).

Tiprelestat, a potent inhibitor of human neutrophil elastase, exhibits antimicrobial and anti-inflammatory properties. It is utilized in the study of inflammation and immune diseases [1].

Lonodelestat TFA (POL6014 TFA) is a potent, selective peptide inhibitor of human neutrophil elastase (hNE), demonstrating oral activity. It holds promise for cystic fibrosis (CF) research [1] [2] [3].

5,7-Dihydroxy-4-methylcoumarin (Methyl-2H-Chromen-2-One) inhibits human neutrophil oxidative metabolism and elastase activity. 5,7-Dihydroxy-4-methylcoumarin has in vitro platelet antiaggregatory property. 5,7-Dihydroxy-4-methylcoumarin shows inhibition of the cyclooxygenase pathway.

Ono EI-601 is the main metabolite of ONO-5046, the human neutrophil elastase inhibitor .

ZD-0892 is a selective and potent inhibitor of neutrophil elastase, inhibits human neutrophil elastase and porcine pancreatic elastase, reverses advanced pulmonary vascular disease produced in rats, and can be used to study chronic obstructive pulmonary disease (COPD) and peripheral vascular disease (PVD).

Sivelestat (ONO5046) is a potent and selective inhibitor of neutrophil elastase with IC50 of 44 nM.

Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent, orally active inhibitor of neutrophil elastase (Ki: 12.2 nM). quarterhydrate is more than 100-fold less active than other proteases such as trypsin, proteinase 3, pancreatic elastase, thrombin, fibrin, collagenase, histone G and murine macrophage elastase, and exhibits potent anti-inflammatory effects.

ICI 200355 is an inhibitor of human neutrophil elastase.

JO146 is a protease inhibitor for Chlamydia trachomatis high temperature requirement A (CtHtrA) and human neutrophil elastase (HNE), with IC50 values of 21.86 μM for CtHtrA and 1.15 μM for HNE, respectively. It is effective in inhibiting bacterial infections.

Elafin, also referred to as elafin-specific inhibitor (ESI) or skin anti-leucoprotease (SKALP), is a protein that serves as a low molecular weight inhibitor of human neutrophil elastase (HNE) and proteinase 3, particularly in the lung. Additionally, Elafin exhibits antibacterial properties against Pseudomonas aeruginosa and Staphylococcus aureus [1] [2] [3].

GW-475151 inhibits human neutrophil elastase (HNE).

MDL 101146 is an orally active neutrophil elastase inhibitor.

MDL-101146, (R)- is an effective orally active inhibitor of human neutrophil elastase.

BAY-678 racemate is a racemate of BAY-678. BAY-678 is an orally bioavailable, selective and cell-permeable inhibitor of human neutrophil elastase (HNE; IC50: 20 nM).

Sivelestat, an inhibitor of human neutrophil elastase, is used in the treatment of acute respiratory failure. Preliminary studies show Sivelestat may improve neuropathic pain.

Ici 186756 is a novel, effective, and selective inhibitor of human neutrophil elastase.

AE-3763 is a peptide-based human neutrophil elastase inhibitor (IC50: 29 nM).

MDL 27324 is an inhibitor of human neutrophil elastase.

BAY-677, serving as an inactive control for BAY-678, is distinguished by BAY-678's capabilities as an orally bioavailable, selective, and cell-permeable inhibitor of human neutrophil elastase (HNE), showcasing a high potency with an IC50 of 20 nM[1]. Furthermore, BAY-678 has been publicly nominated as a chemical probe by the Structural Genomics Consortium (SGC)[2].

Ala-Ala-Pro-Val-chloromethylketone serves as an irreversible inhibitor of human neutrophil elastase (NE), utilized in researching chronic inflammatory airway diseases.

ZD8321 is an effective inhibitor of human Neutrophil elastase (Ki: 13±1.7 nM).

GW-311616 is a long duration, orally bioavailable, and selective human neutrophil elastase (HNE) inhibitor (IC50: 22 nM; Ki: 0.31 nM).

Morolic acid and moronic acid have shown sustained antidiabetic and antihyperglycemic action possibly mediated by an insulin sensitization with consequent changes of glucose, cholesterol and triglycerides, in part mediated by inhibition of 11β-HSD 1. Moro

Midesteine (MR-889) is a small molecule neutrophil elastase inhibitor used in the treatment of bronchitis, asthma and chronic lung disease.

Ici 200880 is a human neutrophil elastase synthetic peptide inhibitor.

Alvelestat (AZD9668) is an orally bioavailable, selective and reversible inhibitor of human neutrophil elastase (NE), with potential anti-inflammatory activity.

Alvelestat can inhibit neutrophil elastase (NE), which acts an important role in NET formation.

Abz-Ala-Pro-Glu-Glu-Ile-Met-Arg-Arg-Gln-EDDnp is a fluorescence-quenched peptide substrate for human neutrophil elastase (kcat/Km = 531 mM-1s-1). Enzymatic peptide hydrolysis disrupts the Abz:EDDnp donor-acceptor pair allowing fluorescence measurement of Abz (ex = 320 nm; em = 420 nm).

KRP-109, a neutrophil elastase (NE) inhibitor, acts by decreasing expression of TGF-ß Signal Related Genes.

Lonodelestat (POL6014) is a potent, orally active and selective peptide inhibitor of human neutrophil elastase (hNE).

Tutuilamide A, a potent inhibitor of porcine pancreatic elastase (PPE) with an IC50 of 1.2 nM, also effectively inhibits human neutrophil elastase (HNE; IC50=0.73 nM) and kallikrein 7 (KLK7; IC50=5.0 nM) [1].

Sivelestat sodium tetrahydrate (ONO5046 sodium tetrahydrate) is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) sodium tetrahydrate has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19.

(R)-BAY-85-8501 is the less active enantiomer of BAY-85-8501. BAY-85-8501 is a selective and potent Human Neutrophil Elastase (HNE)inhibitor(IC50 of 65 pM).

Freselestat (ONO-6818) is a potent neutrophil elastase inhibitor that significantly reduces the production of interleukin 8 and C5B-9. Freselestat reduces inflammatory mediators during simulated cardiopulmonary bypass.

MDL-101146, (S)- is an effective orally active inhibitor of human neutrophil elastase.